Peringatan Keamanan

As lopinavir is only available in combination with ritonavir, experience with acute lopinavir overdose in isolation is limited. The risk related to overdose appears more pronounced in pediatric patients. One case report detailed a fatal cardiogenic shock in a 2.1kg infant following an approximately 10-fold overdose of Kaletra oral solution, while other reported reactions to overdose in infants include complete AV block, cardiomyopathy, lactic acidosis, and acute renal failure. The oral Kaletra solution is highly concentrated, posing a greater risk of overdose, and contains approximately 42% (v/v) ethanol, further increasing risk in children and infants.L11163

There is no antidote for lopinavir overdose. Treatment of overdose should consist largely of supportive measures and close observation of vital signs and clinical status of the affected patient. Consideration should be given to the removal of unabsorbed drug using gastric lavage or activated charcoal, if clinically indicated. Dialysis is unlikely to be of benefit as lopinavir is highly protein-bound, but may help to remove ethanol and propylene glycol from the circulation in the case of overdose with Kaletra oral solution.L11163

Lopinavir

DB01601

small molecule approved

Deskripsi

Lopinavir is an antiretroviral protease inhibitor used in combination with other antiretrovirals in the treatment of HIV-1 infection.L11163 Lopinavir is marketed and administered exclusively in combination with ritonavir - this combination, first marketed by Abbott under the brand name Kaletra in 2000, is necessary due to lopinavir's poor oral bioavailability and extensive biotransformation. Ritonavir is a potent inhibitor of the enzymes responsible for lopinavir metabolism, and its co-administration "boosts" lopinavir exposure and improves antiviral activity.L11163 Like many other protease inhibitors (e.g. saquinavir, nelfinavir), lopinavir is a peptidomimetic molecule - it contains a hydroxyethylene scaffold that mimics the peptide linkage typically targeted by the HIV-1 protease enzyme but which itself cannot be cleaved, thus preventing the activity of the HIV-1 protease.A191757

Lopinavir was previously under investigation in combination with ritonavir for the treatment of COVID-19 caused by SARS-CoV-2.L12012

Struktur Molekul 2D

Berat 628.8008
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of lopinavir is 6.9 ± 2.2 hours.[L11163]
Volume Distribusi The volume of distribution of lopinavir following oral administration is approximately 16.9 L.[L11163]
Klirens (Clearance) The estimated apparent clearance following oral administration is approximately 6-7 L/h.[A191715,L12063]

Absorpsi

When administered alone, lopinavir has exceptionally low oral bioavailability (~25%) - for this reason, it is exclusively co-administered with ritonavir, which dramatically improves bioavailability, hinders drug metabolism, and allows for the attainment of therapeutic lopinavir concentrations.A191715,A191748 Following oral administration of lopinavir/ritonavir, maximal plasma concentrations are achieved at approximately 4.4 hours (Tmax), and the Cmax and AUCtau are 9.8 ± 3.7 - 11.8 ± 3.7 µg/mL and 92.6 ± 36.7 - 154.1 ± 61.4 ?g•h/mL, respectively.L11163 Relative to administration in the fasted state, administration with a meal increases the AUC of the tablet formulation slightly (~19%) but dramatically increases the AUC of the oral solution formulation (~130%).L11163

Metabolisme

Lopinavir undergoes extensive oxidative metabolism, almost exclusively via hepatic CYP3A isozymes.L12063 Co-administration with ritonavir, a potent inhibitor of CYP3A enzymes, helps to stave off lopinavir's biotransformation and increase plasma levels of active antiviral drug. Twelve metabolites have been identified in vitro, with the C-4 oxidation products M1, M3, and M4 being the predominant metabolites found in plasma.A191919 The structures of these primary metabolites have been identified, but precise structural information regarding the remaining minor metabolites has not been elucidated.

Rute Eliminasi

Lopinavir is primarily eliminated in the feces. Following oral administration, approximately 10.4 ± 2.3% of the administered dose is excreted in the urine and 82.6 ± 2.5% is excreted in the feces.L11163 Unchanged parent drug accounted for 2.2% and 19.8% of the administered dose in urine and feces, respectively.L12063

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. Induction of CYP3A by co-administration with St. John's Wort may result in reduced drug plasma concentrations and therapeutic failure.
  • 2. Take with food. The oral solution formulation must be taken with food, but the tablet formulation may be taken with or without food.

Interaksi Obat

1837 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Lopinavir.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Lopinavir.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Lopinavir.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Lopinavir.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Lopinavir.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Lopinavir.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Lopinavir.
Silodosin The excretion of Silodosin can be decreased when combined with Lopinavir.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Lopinavir.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Lopinavir.
Abacavir The serum concentration of Abacavir can be decreased when it is combined with Lopinavir.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Lopinavir.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Lopinavir.
Clarithromycin The serum concentration of Clarithromycin can be increased when it is combined with Lopinavir.
Cyclophosphamide The serum concentration of the active metabolites of Cyclophosphamide can be increased when Cyclophosphamide is used in combination with Lopinavir.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Lopinavir.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Lopinavir.
Nelfinavir The serum concentration of Lopinavir can be decreased when it is combined with Nelfinavir.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Lopinavir.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Lopinavir.
Nevirapine The serum concentration of Lopinavir can be decreased when it is combined with Nevirapine.
Phenytoin The serum concentration of Lopinavir can be decreased when it is combined with Phenytoin.
Fosphenytoin The serum concentration of Lopinavir can be decreased when it is combined with Fosphenytoin.
Methadone Methadone may increase the QTc-prolonging activities of Lopinavir.
Alprazolam The serum concentration of Alprazolam can be increased when it is combined with Lopinavir.
Foscarnet The risk or severity of nephrotoxicity can be increased when Lopinavir is combined with Foscarnet.
Mannitol The risk or severity of nephrotoxicity can be increased when Mannitol is combined with Lopinavir.
Bosentan The serum concentration of Bosentan can be increased when it is combined with Lopinavir.
Vinblastine The serum concentration of Vinblastine can be increased when it is combined with Lopinavir.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Lopinavir.
Vinflunine The serum concentration of Vinflunine can be increased when it is combined with Lopinavir.
Vindesine The serum concentration of Vindesine can be increased when it is combined with Lopinavir.
Vinorelbine The serum concentration of Vinorelbine can be increased when it is combined with Lopinavir.
Vintafolide The serum concentration of Vintafolide can be increased when it is combined with Lopinavir.
Vincamine The serum concentration of Vincamine can be increased when it is combined with Lopinavir.
Voriconazole The serum concentration of Voriconazole can be decreased when it is combined with Lopinavir.
Rifabutin The serum concentration of the active metabolites of Rifabutin can be increased when Rifabutin is used in combination with Lopinavir.
Efavirenz The metabolism of Lopinavir can be increased when combined with Efavirenz.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Lopinavir.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Lopinavir.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Lopinavir.
Didanosine The serum concentration of Didanosine can be decreased when it is combined with Lopinavir.
Quinine The serum concentration of Quinine can be increased when it is combined with Lopinavir.
Quinidine The serum concentration of Quinidine can be increased when it is combined with Lopinavir.
Ketoconazole The serum concentration of Lopinavir can be increased when it is combined with Ketoconazole.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Lopinavir.
Itraconazole The metabolism of Itraconazole can be decreased when combined with Lopinavir.
Saquinavir The serum concentration of Saquinavir can be increased when it is combined with Lopinavir.
Darunavir The serum concentration of Darunavir can be decreased when it is combined with Lopinavir.
Amprenavir The serum concentration of Lopinavir can be decreased when it is combined with Amprenavir.
Fosamprenavir The serum concentration of Lopinavir can be decreased when it is combined with Fosamprenavir.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Lopinavir.
Garlic Garlic can cause a decrease in the absorption of Lopinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Icosapent The risk or severity of nephrotoxicity can be increased when Icosapent is combined with Lopinavir.
Cefotiam The risk or severity of nephrotoxicity can be increased when Cefotiam is combined with Lopinavir.
Mesalazine The risk or severity of nephrotoxicity can be increased when Mesalazine is combined with Lopinavir.
Cefmenoxime The risk or severity of nephrotoxicity can be increased when Cefmenoxime is combined with Lopinavir.
Cefmetazole The risk or severity of nephrotoxicity can be increased when Cefmetazole is combined with Lopinavir.
Triamterene The risk or severity of nephrotoxicity can be increased when Triamterene is combined with Lopinavir.
Cefpiramide The risk or severity of nephrotoxicity can be increased when Cefpiramide is combined with Lopinavir.
Loracarbef The risk or severity of nephrotoxicity can be increased when Loracarbef is combined with Lopinavir.
Cefalotin The risk or severity of nephrotoxicity can be increased when Cefalotin is combined with Lopinavir.
Nabumetone The risk or severity of nephrotoxicity can be increased when Nabumetone is combined with Lopinavir.
Tenoxicam The risk or severity of nephrotoxicity can be increased when Tenoxicam is combined with Lopinavir.
Cefotaxime The risk or severity of nephrotoxicity can be increased when Cefotaxime is combined with Lopinavir.
Tolmetin The risk or severity of nephrotoxicity can be increased when Tolmetin is combined with Lopinavir.
Fenoprofen The risk or severity of nephrotoxicity can be increased when Fenoprofen is combined with Lopinavir.
Sulindac The risk or severity of nephrotoxicity can be increased when Sulindac is combined with Lopinavir.
Bacitracin The risk or severity of nephrotoxicity can be increased when Bacitracin is combined with Lopinavir.
Cephaloglycin The risk or severity of nephrotoxicity can be increased when Cephaloglycin is combined with Lopinavir.
Adefovir dipivoxil The risk or severity of nephrotoxicity can be increased when Adefovir dipivoxil is combined with Lopinavir.
Carprofen The risk or severity of nephrotoxicity can be increased when Carprofen is combined with Lopinavir.
Etacrynic acid The risk or severity of nephrotoxicity can be increased when Etacrynic acid is combined with Lopinavir.
Ceforanide The risk or severity of nephrotoxicity can be increased when Ceforanide is combined with Lopinavir.
Salicylic acid The risk or severity of nephrotoxicity can be increased when Salicylic acid is combined with Lopinavir.
Balsalazide The risk or severity of nephrotoxicity can be increased when Balsalazide is combined with Lopinavir.
Cefditoren The risk or severity of nephrotoxicity can be increased when Cefditoren is combined with Lopinavir.
Colistimethate The risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Lopinavir.
Cefuroxime The risk or severity of nephrotoxicity can be increased when Cefuroxime is combined with Lopinavir.
Cefapirin The risk or severity of nephrotoxicity can be increased when Cefapirin is combined with Lopinavir.
Cefprozil The risk or severity of nephrotoxicity can be increased when Cefprozil is combined with Lopinavir.
Olsalazine The risk or severity of nephrotoxicity can be increased when Lopinavir is combined with Olsalazine.
Lumiracoxib The risk or severity of nephrotoxicity can be increased when Lumiracoxib is combined with Lopinavir.
Cefamandole The risk or severity of nephrotoxicity can be increased when Cefamandole is combined with Lopinavir.
Cefazolin The risk or severity of nephrotoxicity can be increased when Cefazolin is combined with Lopinavir.
Cefonicid The risk or severity of nephrotoxicity can be increased when Cefonicid is combined with Lopinavir.
Cefoperazone The risk or severity of nephrotoxicity can be increased when Cefoperazone is combined with Lopinavir.
Cefoxitin The risk or severity of nephrotoxicity can be increased when Cefoxitin is combined with Lopinavir.
Ceftizoxime The risk or severity of nephrotoxicity can be increased when Ceftizoxime is combined with Lopinavir.
Magnesium salicylate The risk or severity of nephrotoxicity can be increased when Magnesium salicylate is combined with Lopinavir.
Salsalate The risk or severity of nephrotoxicity can be increased when Salsalate is combined with Lopinavir.
Choline magnesium trisalicylate The risk or severity of nephrotoxicity can be increased when Choline magnesium trisalicylate is combined with Lopinavir.
Cefepime The risk or severity of nephrotoxicity can be increased when Cefepime is combined with Lopinavir.
Cefacetrile The risk or severity of nephrotoxicity can be increased when Cefacetrile is combined with Lopinavir.
Cefpodoxime The risk or severity of nephrotoxicity can be increased when Cefpodoxime is combined with Lopinavir.
Antrafenine The risk or severity of nephrotoxicity can be increased when Antrafenine is combined with Lopinavir.
Tiaprofenic acid The risk or severity of nephrotoxicity can be increased when Tiaprofenic acid is combined with Lopinavir.
Hydrolyzed Cephalothin The risk or severity of nephrotoxicity can be increased when Lopinavir is combined with Hydrolyzed Cephalothin.
Cephalothin Group The risk or severity of nephrotoxicity can be increased when Lopinavir is combined with Cephalothin Group.
Oxyphenbutazone The risk or severity of nephrotoxicity can be increased when Lopinavir is combined with Oxyphenbutazone.

Target Protein

Pol polyprotein pol

Referensi & Sumber

Artikel (PubMed)
  • PMID: 21953914
    Li F, Lu J, Ma X: CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. Drug Metab Dispos. 2012 Jan;40(1):18-24. doi: 10.1124/dmd.111.041400. Epub 2011 Sep 27.
  • PMID: 22762019
    Sundquist WI, Krausslich HG: HIV-1 assembly, budding, and maturation. Cold Spring Harb Perspect Med. 2012 Jul;2(7):a006924. doi: 10.1101/cshperspect.a006924.
  • PMID: 30346663
    Niu WJ, Sun T, Liu L, Liu XQ, Zhang RF, Yin L, Wang JR, Jia XF, Lu HZ, Zhong MK, Jiao Z, Zhang LJ: Population pharmacokinetics and dosing regimen optimisation of lopinavir in Chinese adults infected with HIV. Basic Clin Pharmacol Toxicol. 2019 Apr;124(4):456-465. doi: 10.1111/bcpt.13154. Epub 2018 Nov 23.
  • PMID: 9835517
    Sham HL, Kempf DJ, Molla A, Marsh KC, Kumar GN, Chen CM, Kati W, Stewart K, Lal R, Hsu A, Betebenner D, Korneyeva M, Vasavanonda S, McDonald E, Saldivar A, Wideburg N, Chen X, Niu P, Park C, Jayanti V, Grabowski B, Granneman GR, Sun E, Japour AJ, Leonard JM, Plattner JJ, Norbeck DW: ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24.
  • PMID: 19108994
    De Clercq E: Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV. Int J Antimicrob Agents. 2009 Apr;33(4):307-20. doi: 10.1016/j.ijantimicag.2008.10.010. Epub 2008 Dec 23.
  • PMID: 9884314
    Kumar GN, Jayanti V, Lee RD, Whittern DN, Uchic J, Thomas S, Johnson P, Grabowski B, Sham H, Betebenner D, Kempf DJ, Denissen JF: In vitro metabolism of the HIV-1 protease inhibitor ABT-378: species comparison and metabolite identification. Drug Metab Dispos. 1999 Jan;27(1):86-91.

Contoh Produk & Brand

Produk: 49 • International brands: 2
Produk
  • Kaletra
    Tablet, film coated • - • Oral • US • Approved
  • Kaletra
    Tablet, film coated • - • Oral • US • Approved
  • Kaletra
    Tablet, film coated • - • Oral • US • Approved
  • Kaletra
    Tablet, film coated • - • Oral • US • Approved
  • Kaletra
    Tablet, film coated • - • Oral • US • Approved
  • Kaletra
    Tablet • - • Oral • US
  • Kaletra
    Tablet, film coated • - • Oral • US • Approved
  • Kaletra
    Tablet, film coated • - • Oral • US • Approved
Menampilkan 8 dari 49 produk.
International Brands
  • Aluviran
  • Koletra

Sekuens Gen/Protein (FASTA)

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